SINGULAIR (Montelukast)

Brand name: SINGULAIR

Generic name: montelukast

Dosage form: coated tablets / chewable tablets

Ingredients:

A film-coated tablet contains:
Active ingredient: montelukast - 10 mg;
Excipients: microcrystalline cellulose, lactose, sodium croscarmellose, giproloza, magnesium stearate.
Composition of the membrane covering the pill: giproloza, hypromellose, titanium dioxide, dyes, iron oxide red and iron oxide yellow, and carnauba wax.
1 tablet chewable contains:
Active ingredient: montelukast - 5 mg;
Excipients: mannitol, microcrystalline cellulose, giproloza, stain iron oxide red, croscarmellose sodium, cherry flavor, aspartame and magnesium stearate.

Description:

Tablets 10 mg coated tablets: light cream, square pill with rounded edges, coated, engraved with «MSD 117" on one side and «SINGULAIR» on the other side.
Chewable Tablets 5 mg: pink, round, biconvex tablets embossed with the inscription «MSD 275" on one side and «SINGULAIR» on the other side.

Pharmacotherapeutic group: a leukotriene-receptor blocker.

ATC code: R03DC03

Pharmacological properties:

Pharmacodynamics

Montelukast inhibits cysteinyl leukotriene-receptor epithelium of the respiratory tract, thus having both the ability to inhibit bronchoconstriction due to inhalation of cysteinyl-leukotriene LTD4 in patients with asthma. 5 mg is enough to relieve the bronchospasm induced LTD4. Use of montelukast in doses exceeding 10 mg per day, taken singly, the effectiveness of the drug did not increase.
Montelukast causes bronchodilation within 2 hours after ingestion, and may complement the bronchodilation caused by ?2-adrenomimetikami.

Pharmacokinetics

Suction

Montelukast rapidly and almost completely absorbed after oral administration. Receiving regular food does not affect the bioavailability and maximum plasma concentration (Cmax) of tablets coated and chewable tablets. In adults, when receiving an empty stomach tablets coated tablets 10 mg Cmax achieved in 3 hours. Oral bioavailability is 64%.
When you receive an empty stomach tablets chewable 5 mg Cmax adults reached in 2 hours. Bioavailability is 73%.

Distribution

Montelukast binds to plasma proteins more than 99%. The volume of distribution of montelukast averages 11.8 liters.

Metabolism

Montelukast is actively metabolized in the liver. When using therapeutic doses of the concentration of metabolites of montelukast in plasma at steady state in adults and children is not determined.
It is assumed that the metabolism of montelukast involve cytochrome P450 isoenzymes CYP (3A4 and 2C9), with therapeutic concentrations of montelukast do not inhibit cytochrome P450 isoenzymes CYP: 3A4, 2C9, 1A2, 2A6, 2S19, and 2D6.

Breeding

Clearance of montelukast in healthy adults an average of 45 ml / min. Following oral administration of montelukast, 86% of the amount excreted in the feces within 5 days and less than 0,2% - in the urine, confirming that montelukast and its metabolites are excreted almost exclusively in bile.
The half-life of montelukast in young healthy adults ranges from 2,7 to 5,5 hours. The pharmacokinetics of montelukast retains almost linear with the ingestion of doses exceeding 50 mg. When receiving montelukast in the morning and evening hours pharmacokinetic differences are not observed. When you receive a once-daily tablets coated tablets of 10 mg observed moderate (14%) accumulation of the active substance in the plasma.

Peculiarities of the pharmacokinetics in different patient groups

Paul
Pharmacokinetics of montelukast in men and women is similar.
Elderly patients
When ingestion of a once-daily tablet coated 10 mg pharmacokinetic profile and bioavailability are similar in elderly and younger patients.
Hepatic failure
In patients with hepatic insufficiency mild to moderate severity and clinical manifestations of liver cirrhosis observed slowing of metabolism of montelukast, accompanied by an increase in area under the pharmacokinetic curve "concentration-time» (AUC) by approximately 41% after a single dose of the drug at a dose of 10 mg. Elimination of montelukast in these patients, a slight increase compared with healthy subjects (mean half-life - 7.4 hours). Change the dose of montelukast for patients with hepatic insufficiency mild to moderate severity is not required. Data on the nature of the pharmacokinetics of montelukast in patients with severe hepatic insufficiency (more than 9 points on the Child-Pugh) do not.
Race
There were no differences in clinically significant pharmacokinetic effects in patients of different races.
Renal failure
Because montelukast and its metabolites are not excreted in the urine, the pharmacokinetics of montelukast in patients with renal failure was not evaluated. Adjustment of the dose for this group of patients is required.

Indications:

Prevention and long-term treatment of asthma in adults and children from 6 years, including the prevention of daytime and nighttime symptoms, treatment of aspirin in patients with bronchial asthma and the prevention of bronchospasm caused by exercise.
Relief of daytime and nighttime symptoms of seasonal allergic rhinitis (adults and children 6 years old) and perennial allergic rhinitis (adults and children 6 years old)
Contraindications:
Hypersensitivity to any component of the drug.
Children under 6 years old.
Application of pregnancy and lactation:

SINGULAIR should be used during pregnancy and lactation unless the expected benefit to the mother justifies the potential risk to the fetus or child.

Dosage and administration:

Inward 1 time per day regardless of meals. For the treatment of bronchial asthma singular should be taken in the evening. In the treatment of allergic rhinitis dose may be taken at any time at the request of the patient. Patients suffering from bronchial asthma and allergic rhinitis should take one tablet once a singular day in the evening.
Adults aged 15 and older
The dose for adults and children over 15 years is a coated tablets of 10 mg per day.
Children aged 6 to 14 years
The dosage for children 6-14 years is one tablet, chewing 5 mg per day. Selection of doses for this age group is not required.

General Recommendations

The therapeutic effect of SINGULAIR on parameters reflecting the course of bronchial asthma develops during the first day. The patient should continue taking SINGULAIR in the period to achieve control of symptoms of asthma and in exacerbation of asthma.
For elderly patients, patients with renal insufficiency, and patients with mild to moderate liver dysfunction, and depending on the sex of a special selection of a dose is not required.
Appointment of SINGULAIR in conjunction with other forms of treatment of bronchial asthma
SINGULAIR can be added to the treatment of patients with bronchodilators and inhaled corticosteroids (See "Interaction with other drugs).

Side effects:

In general, SINGULAIR was well tolerated. Side effects are usually mild and usually do not require discontinuation of treatment. The overall incidence of side effects reported with use of SINGULAIR, is comparable to that for placebo:
hypersensitivity reactions (including anaphylaxis, angioedema, rash, pruritus, urticaria and rarely eosinophilic infiltration of the liver); uzelklvuyu erythema, weird vivid dreams, hallucinations, drowsiness, irritability, agitation, including aggressive behavior, fatigue, suicidal thoughts and suicidal behavior (suicidality ), insomnia, paraesthesia / hypoesthesia, very rarely - seizures, nausea, vomiting, diarrhea, abdominal pain, headache, arthralgia, myalgia, muscle cramps, tendency to increased bleeding, formation of subcutaneous hemorrhage, palpitation, edema.

Overdose:

Data on overdose symptoms while taking SINGULAIR patients with asthma in a dose exceeding 200 mg / day for 22 weeks and a dose of 900 mg / day for 1 week was not revealed.
There have been reports of acute overdose of montelukast in children (receiving no less than 150 mg a day). Clinical and laboratory data at this show under the safety profile of SINGULAIR in children safety profile in adults and elderly patients. The most common adverse events were thirst, somnolence, mydriasis, hyperkinesis, and abdominal pain.
Treatment is symptomatic.
Data on the possibility of removing montelukast by peritoneal dialysis or hemodialysis not.

Interaction with other drugs:

SINGULAIR may be given together with other drugs, traditionally used for prevention and long-term treatment of bronchial asthma. The recommended clinical dose of montelukast has no clinically significant effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol / norethindrone 35 / 1), terfenadine, digoxin and warfarin.
AUC decreased in patients while receiving phenobarbital (approximately 40%), but the correction SINGULAIR dosage regimen in such patients is required.
Treatment with bronchodilators: SINGULAIR can be added to the treatment of patients whose asthma is not controlled using one bronchodilator. Upon reaching the therapeutic effect (usually after the first dose) during therapy with SINGULAIR, a dose of bronchodilator can be gradually reduced.
Inhaled corticosteroids: Treatment SINGULAIR provides an additional therapeutic effect to patients receiving treatment with inhaled corticosteroids. Upon reaching the stabilization of the patient may decrease the dose of corticosteroids. Dose of corticosteroids to reduce gradually under medical supervision. Some patients taking inhaled corticosteroids can be completely abolished. Not recommended sharp replacement therapy with inhaled corticosteroids purpose is singular.

Special instructions:

SINGULAIR tablets is not recommended for treatment of acute asthma attacks. In acute bronchial asthma patients should be prescribed drugs for relieves and prevents asthma therapy.
Dose used in conjunction with SINGULAIR inhaled glucocorticosteroids can be gradually reduced under the supervision of a physician. SINGULAIR can dramatically change an inhaled or oral corticosteroids.
Reducing the dose of systemic corticosteroids in patients receiving anti-asthma product, including leukotriene-receptor blockers, followed by a rare appearance of one or more of the following effects: eosinophilia, vascular rash, worsening pulmonary symptoms, cardiac complications and / or neuropathy sometimes diagnosed as a syndrome Chargoi -Straus - eosinophilic systemic vasculitis. Although the causal relationship of these adverse events with therapy leukotriene-receptor antagonist has not been established at lower doses of systemic corticosteroids in patients receiving SINGULAIR should exercise caution and conduct the appropriate clinical follow-up.
Use in elderly patients
Age differences in the profiles of efficacy and safety of SINGULAIR is not revealed.

Effects on ability to drive or moving machinery.

Evidence that taking SINGULAIR affect your ability to drive or moving mechanisms have been identified.

Product:

Chewable Tablets 5 mg or 10 mg tablets, coated tablets.
To 7 chewable tablets 5 mg or 7 tablets 10 mg, coated tablets are placed in a blister.
1, 2 or 4 blisters, along with instructions for use is placed in a cardboard box.

Storage Conditions:

List B.
At a temperature not exceeding 30 ° C and protected from moisture and light and the reach of children.

Expiration date:

Shelf life for chewable tablets 5 mg - 2 years.
Shelf life for the coated tablets 10 mg - 3 years.
Do not use after expiration date printed on the package.

Conditions of supply of pharmacies:

Prescription.